Drug intelligence / Profile preview

gefitinib + pemetrexed + carboplatin

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral (gefitinib), Intravenous (pemetrexed, Carboplatin)
01

Overview

A combination regimen of **gefitinib** (an oral first-generation epidermal growth factor receptor tyrosine kinase inhibitor), **pemetrexed** (an antifolate antineoplastic agent), and **carboplatin** (a platinum-based chemotherapeutic), primarily used as first-line therapy for advanced **non–small cell lung cancer (NSCLC)** harboring *EGFR*-sensitizing mutations. - **Mechanism of Action:** Gefitinib inhibits the kinase activity of the epidermal growth factor receptor (EGFR), thereby blocking tumor cell proliferation and survival. Pemetrexed inhibits multiple enzymes involved in folate-dependent DNA synthesis and replication, suppressing cell division. Carboplatin induces DNA crosslinking and damage, leading to apoptosis in rapidly dividing cells. - **Indication:** First-line treatment for patients with advanced NSCLC with activating EGFR mutations[1][2][3][4][5][6][7][8]. - **Efficacy:** The combination demonstrates synergistic antitumor effects, significantly improving progression-free survival (PFS), overall survival (OS), and objective response rate (ORR) compared to gefitinib alone, with tolerable but increased toxicities (notably, hematologic and gastrointestinal)[1][3][4][5][6][7][8].

Brand names
IressaAlimtaParaplatin
Other names
PC plus gefitinibgefitinib + PCgefitinib plus pemetrexed and carboplatin chemotherapy
02

Targets

GART (GAR transformylase)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)DNAEGFR (Epidermal growth factor receptor)

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